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Adrenergic rem.ppt pharma adrenergeic receptos mechanism
- 1. Adrenergic remedies Lecture byRaychan K. Stikeyeva Higher doctorate
- 2. Adrenergic remedies β β α α α α нана на на Фа На МАО КОМТ на на на
- 4. α-receptors: Vessels of theskin, mucous membranes of the brain - the restriction Radial arm pupil - mydriasis Salivary glands - secretions thickening β-receptors: β 1-heart - quickening rhythm, increasing contractility, conduction, automaticity β 2 - bronchial and skeletal muscles - relaxation α and β-receptors: GIT α2 and β2- lowering tone and peristalsis α - reduction of sphincter Bladder - reduction in detrusor’s relaxation Receptacles: α - the restriction β2 - extension Adipocytes α2 and β1 - lipolysis Hepatocytes α and β2-glycogenolysis, neoglyukogenez Platelets α2- aggregation
- 5. Classification of Adrenergicremedies I. Adrenergic agonists (adrenomimetics) 1) α, β-Adrenomimetics (α1, α2, β1, β2, β3) • direct action – epinephrine (adrenaline) • indirect action) – ephedrine 2) α-Adrenomimetics • non-selective α1, α2 β1 mimetic - norepinephrine • selective adrenergic agonists - phenylephrine (mesaton) (α1), naphazoline (α2), xylometazoline (galazolin) (α2) 3) β-Adrenomimetics • non-selective β1, β2 -mimetics- isoprenaline (izadrin) • selective β2-mimetics: salbutamol, salmeterol, terbutaline, fenoterol, formoterol; β3 -mimetics– mirabegron 4) Dopaminergic catecholamines: dopamine (α1β1, D-mimetic), dobutamine (β1, α1 β2- mimetic) II. Adrenergic blockers 1) α -Adrenoblockers: • non-selective α1, α2 adrenergic blockers - phentolamine • selective α1 blockers - prazosin, doxazosin 2) β -Adrenoblockers: • non-selective β1, β2 adrenergic blockers - propranolol • selective β1 blockers - atenolol, metoprolol, bisoprolol 3) Sympatholytics: octadine, reserpine
- 6. adrenaline Adenylate cyclase АТP cАМP • Antiallergic action •Bronchodilator action • Vasoconstrictor action • Cardiotonic action Change in enzyme activity ++ Сa Proteinkinase Α-β-adrenoceptor agonists - Adrenaline hydrochloride
- 7. The effect ofadrenaline In acting on α- adrenergic receptors narrows most blood vessels increases blood pressure Stimulating of the radial muscles of iris - m. dilatator pupillae - mydriasis Reduction of splenic capsule
- 8. The effects associatedwith the action of adrenaline on the beta-adrenergic receptors β1-adrenoreceptors: - increases cardiac contractility (positive inotropic effect); - Increased frequency of contractions (positive chronotropic effect); - Improves conductivity (positive dromotropic effect); - Increases automaticity (bathmotropic positive effect). β2-adrenergic receptors Bronchodilation effect Dilatation under the action of adrenaline coronary, pulmonary vessels, vessels of skeletal muscle, brain. β1 and β2,3-adrenoceptor stimulates glycogenolysis (hyperglycemia). reduces the secretion of glands tracheobronchial tree a weak stimulating effect on CNS
- 9. indications for theusage of Adrenaline acute hypotension, collapse, anaphylactic shock, bronchospasm, with local anaesthetics to extend their effect and reduce the toxicity AV - heart block hypoglycemic coma. Side effects of adrenalin cardiac arrhythmias, such as ventricular fibrillation Easy anxiety, tremor, agitation. pulmonary edema
- 10. Ephedrine hydrochloride Side effects Increasedblood pressure Palpitations, tachycardia Angina Headache Tremor, tension Excitement, confusion Sleep Disorders Psychosis, hallucinations depression tachyphylaxis phenomenon
- 11. indications for theusage of Ephedrine bronchial asthma chronic hypotension Rhinitis AV-block narcolepsy poisoning with hypnotics and narcotics
- 12. Noradrenaline hydrotartratis (Norepinephrine) The main effect -increase in blood pressure due to a direct stimulating effect on α-receptors on blood vessels and increasing the peripheral resistance On smooth muscles of internal organs, metabolism and CNS drug has a one-way action with adrenaline, but significantly inferior to the latter. The main route of administration of norepinephrine –I/V INDICATIONS of Noradrenaline: shock, except cardiogenic and hemorrhagic. ADVERSE REACTIONS : 1) respiratory failure; 2) headache; 3) cardiac arrhythmias 4) on-site injection may cause tissue necrosis
- 13. β-adrenomimetics Pharmacological effects ofIzadrine Exciting β2-adrenergic receptors of bronchi, bronchodilation effect promotes ejection of the mucous glands of water (dilution of sputum),activation of mucociliary transport. Exciting β1-Adrenergic receptors of heart reduces pulmonary and systemic vascular resistance Exciting β2-adrenergic receptors leads to a relaxation of the muscles of the uterus. Stimulates the central nervous system, metabolism effects similar to adrenaline INDICATIONS FOR USE asthma attacks AV-blockade for muscle relaxation of the uterus - tocolytic effect. SIDE EFFECTS: Tachycardia, palpitation, arrhythmias, headache, Tremor,
- 14. Selective β2-adrenoceptor agonists:salbutamol, fenoterol, terbutaline stimulating effect on the β2-adrenergic drugs are effective for enteral application and compared with izadrine their effect persists for a longer time. INDICATIONS: 1) bronchial asthma (inhalation, orally, parenterally); 2) to reduce the contractile activity of myometrium (tocolytics) to prevent preterm birth.
- 15. Adrenoblockers Indications for theusage. Phentolamine currently use is relatively rare: 1) pheochromocytoma; 2) endarteritis, acrocyanosis, trophic ulcers 3) hemorrhagic, cardiogenic shock, 4) hypertensive crisis 5) frostbite. Blockade of α 2-presynaptic receptors Associated with this SIDE EFFECTS: -Tachycardia; - diarrhoea ; - Dizziness; - Itching,; - Swelling of the mucous membranes of the nose; - Overdose - orthostatic collapse.
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- 17. β - blockers Block ofβ-adrenergic receptors of the juxtaglomerular apparatus of the kidneys Block of presynaptic β-adrenergic receptors of vessels Inhibition of the central links of the sympathetic nervous system Decreased secretion of renin Decreased tone of peripheral vessels Hypotensive effect Antianginal effect Antiarrhythmic effect Block of β-adrenergic receptors of the heart Decreased strength and heart rate Decreased automatism, conduction and excitability of the myocardium Reduction of shock and minute ejection Decreased oxygen demand of the heart β-adrenoblockers: propranolol, oxprenolol, pindolol, sotalol, acebutalol, sectral, trasicor, timolol, atenolol INDICATIONS: •angina pectoris •atrial tachyarrhythmia s • tachycardias •Hypertension •glaucoma
- 18. PHARMACOLOGICAL EFFECTS OF selectiveaction β1- adrenoblockers. On the example of Propranolol Blocking β1-adrenergic receptors, propranolol reduces myocardial contractility, suppress automaticity and slows atrioventricular conduction, and decreases excitability (antiarrhythmic action). Decreases myocardial oxygen demand and improves exercise tolerance in patients with angina (antianginal). Reduced pumping function of the heart causes a reduction in blood pressure (hypotensive effect). Hypotensive effect also contributes to the fact that Inderal lowers renin activity (reduces the production of it) and has a central hypotensive action.
- 20. Thank youfor attention